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On-DNA Pd and Cu promoted C-N cross-coupling reactions.

ABSTRACT: Encoded library technology (ELT) is a novel hit identification platform synergistic with HTS, fragment hit ID and focused screening. It provides both an ultra high-throughput and a cost-efficient tool for the discovery of small molecules that bind to protein targets of pharmaceutical interest. The success of ELT relies heavily on the chemical diversity accessed through DNA-encoded library (DEL) synthesis. We developed unprecedented Pd and Cu(i) promoted C-N cross-coupling reactions between a DNA-conjugated aryl iodide and primary amines. These reported reactions have strong potential for application in DNA-encoded library (DEL) synthesis.

SUBMITTER: Lu X

PROVIDER: S-EPMC6072107 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature

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On-DNA Pd and Cu promoted C-N cross-coupling reactions.

Lu Xiaojie X Roberts Sarah E SE Franklin George J GJ Davie Christopher P CP

MedChemComm 20170712 8

Encoded library technology (ELT) is a novel hit identification platform synergistic with HTS, fragment hit ID and focused screening. It provides both an ultra high-throughput and a cost-efficient tool for the discovery of small molecules that bind to protein targets of pharmaceutical interest. The success of ELT relies heavily on the chemical diversity accessed through DNA-encoded library (DEL) synthesis. We developed unprecedented Pd and Cu(i) promoted C-N cross-coupling reactions between a DNA ...[more]

PMID: 30108872

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